Choleretic and cholekinetic drugs - Pharmacology

Choleretic and cholekinetic agents

With liver pathology, there is often a need to strengthen and alleviate the secretion of the liver - bile. In these cases, cholagogue is used. The biliary tract is shown in Fig. 6.8.

Bile contains bile acids, which emulsify fats in the intestine and promote their absorption, as well as fat-soluble vitamins. Lack of bile may be associated with a violation of its formation in liver cells or with difficulty in entering the duodenum from the bile ducts.

The cholagogue funds are conventionally divided into two groups: bile secretion enhancing agents ( choleretic agents ) and promoting the release of bile into the intestine ( cholekinetic means).

Scheme of bile ducts

Fig. 6.8. Scheme of bile ducts:

1 - bile intrahepatic ducts; 2 - common hepatic duct; 3 - gall bladder; 4 - bladder duct; 5 - common bile duct; 6 - duodenum

Cholekinetic drugs, in turn, are represented by two groups of substances: hyperquatic drugs (causing a contraction of the gallbladder) and hypochinetic (i) eliminating the spasm of bile duct sphincters (cholespasmolytics). Some agents combine different types of activity.

Particularly strong stimulants of bile secretion are bile acids. The drug & quot; Holenzyme & quot; (contains bile, pancreatic powder and mucosa of the small intestine powder) this also combines the function of substitution therapy. In the preparation & quot; Allochol & quot; (contains activated charcoal, bile, nettle leaves nettle and of the onion seed garlic) the stimulating effect of bile is combined with the plant choleretic components.

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Magnesium sulfate, which is injected through the probe into the duodenum, causes reflex reduction of the gallbladder and relaxation of the sphincter of Oddi.

Cholagogue is used for chronic hepatitis, cholangitis, chronic cholecystitis. Pharmacological classification of cholagogue agents is presented in Table. 6.4.

Table 6.4

Pharmacological classification of cholagogue funds

Group

Drugs

Bile secretion enhancing agents (choleretics)

Bile acids and preparations containing them: dehydrocholic acid (& quot; Cholagol & quot;),

Combined: & quot; Allochol & quot ;, & quot; Cholenzyme & quot ;.

Synthetic preparations: ademethionine * (& quot; Heptral & quot;). Herbal remedies: corn stalks with stigmas, immortelle sandy flowers , etc.

Means that enhance the secretion of bile (cholekinetics)

Hyperkinetics: magnesium sulfate. Polyhydric alcohols: xylitol, manite

Hypokinetics (cholespasmolytics): atropine and similar preparations.

Myotropic (papaverine-like) drugs

Medications that combine choleretic and cholekinetic effects

Sorbitol, tansy of ordinary flowers , artichoke leaves extract (& quot; Hofitol & quot;)

Medications that combine choleretic and hypokinetic (spasmolytic) action

Rosehip hips extract (Holosas), sandwich flowers immortal sum of flavonoids (& quot; Flamin & quot;), hymecromone (& quot; Odeston & quot;).

Combination drugs: & quot; Chalagol & quot;

Ademetionine is a part of all tissues and body fluids, where it participates in transmethylation reactions as a methyl group donor, a precursor of thiol compounds (cysteine, taurine, glutathione, CoA). It is used for intrahepatic cholestasis with precirrotic and cirrhotic conditions.

The connection of the pancreas, liver and bile ducts is shown in Fig. 6.9.

Pancreas, liver and bile ducts connectivity

Fig. 6.9. Connections of the pancreas, liver and bile ducts

& quot; Choleretic levy # 2 & quot; and & quot; Cholagogue collection No. 3 & quot; prescribe as a part of complex therapy with acalculous cholecystitis, chronic hepatitis, dyskinesia of bile ducts.

Choleretics include drugs that dissolve the cholesterol stones that appeared in the gallbladder. The composition of the gall bladder is presented in Table. 6.5.

Composition of the gallbladder

Table 6.5

Bile components

Content in bile

Water

85.9%

Bile acids

98-196 mmol/l

Lecithin

0.51 mmol/l

Total protein

3.15-5.39 g/l

Cholesterol

2.58-23.27 mmol/l

Bilirubin

0.855-17.1 mmol/l

There are known individual drugs that can cause dissolution in the gallbladder of small cholesterol stones (containing calcium salts less than 4%). Natural ursodeoxycholic acid (& quot; Livedaxa & quot ;, & quot; Ursofalk & quot;) has this property. Their use leads to a decrease in the concentration of cholesterol in the bile. For chenodeoxycholic acid, this is due to the inhibition of cholesterol synthesis in hepatocytes. Ursodeoxycholic acid lowers the absorption of endogenous and exogenous cholesterol in the intestine, and also inhibits the production of cholesterol in the liver. The decrease in bile level of cholesterol that occurs under the influence of drugs reduces the probability of formation of cholesterol stones in the gallbladder. At the same time, a change in the ratio between the content of bile cholesterol and bile acids in the bile promotes the gradual dissolution of cholesterol stones.

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These cholelitholitic agents are effective only in a part of patients with long-term use (1 year or more), maintenance therapy - up to 2 years. Enter them inside. From adverse effects, diarrhea, an increase in the level of aminotransferase, skin itching, etc. are noted. Side effects often cause chenodeoxycholic acid. Therefore, it is more appropriate to use ursodeoxycholic acid, but this is a more expensive drug. Sometimes both bile acids are combined. In addition to using these drugs to dissolve cholesterol stones, ursodeoxycholic acid is also prescribed for biliary cirrhosis.

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